TGFβRI-IN-2 is a selective, potent and orally active inhibitor of (Activin-Like Kinase 5) ALK 5(pIC50 and pEC50 values of 7.6 and 6.63, respectively).

Umbralisib R-enantiomer exhibits IC50 with respect to the δ type PI3-kinase that is at least 20-fold lower than the inhibitor's IC50 with respect to the rest of the other PI3K isoforms (i.e., a, β, and γ).

TGFβRI-IN-2 oral administation with 50, 150 and 500 mg/kg and 5 days induces cardiovascular toxicity characterized by valvular interstitial cell proliferation, neutrophil presence, hemorrhage and fibrin deposition in the heart valves.

1976038-41-1

C20H15ClFN5O2

411.82

TGFβRI-IN-2;TP-008

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years